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Assay Detail

CHEMBL2406871

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antitrypanosomal activity against blood stream form of Trypanosoma brucei brucei
17
Total Activities
15
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.
Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.
J Med Chem (2013) 56 : 5637 -5658
PubMed 23611656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
ED50 10 7.33 7.75
IC50 5 5.03 5.44
MIC 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406405 2 7.75
CHEMBL177914 2 7.35
CHEMBL265502 SURAMIN 3.0 1 6.89
CHEMBL128221 1 5.44
CHEMBL426774 1 5.32
CHEMBL2179950 1 5.21
CHEMBL2402202 1 4.68
CHEMBL2402203 1 4.51
CHEMBL604079 1 -
CHEMBL604281 1 -
CHEMBL327624 1 -
CHEMBL594719 1 -
CHEMBL2402190 1 -
CHEMBL604078 1 -
CHEMBL91704 K-777 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406405 ED50 = 18.0 nM 7.75
CHEMBL177914 ED50 = 45.0 nM 7.35
CHEMBL265502 SURAMIN ED50 = 130.0 nM 6.89
CHEMBL128221 IC50 = 3600.0 nM 5.44
CHEMBL426774 IC50 = 4800.0 nM 5.32
CHEMBL2179950 IC50 = 6100.0 nM 5.21
CHEMBL2402202 IC50 = 21000.0 nM 4.68
CHEMBL2402203 IC50 = 31000.0 nM 4.51
CHEMBL604079 ED50 - -
CHEMBL604281 ED50 - -
CHEMBL177914 MIC = 100000.0 nM -
CHEMBL327624 ED50 = 5.6 uM -
CHEMBL594719 ED50 = 1.4 uM -
CHEMBL2402190 ED50 = 1.2 uM -
CHEMBL604078 ED50 = 1.1 uM -
CHEMBL91704 K-777 ED50 = 0.9 uM -
CHEMBL406405 MIC = 10000.0 nM -